Preclinical Development of MiBIECT, a New Oxadiazolyl-Oxazolidinone Compound Active against Gram-positive Cocci

Autor: MUSUMECI, ROSARIO, BULBARELLI, ALESSANDRA, SANCINI, GIULIO ALFREDO, COCUZZA, CLEMENTINA ELVEZIA, Wiederhold, NP, Jorgensen, JH, Patterson, TF, Pace, A, Palumbo Piccionello, A, Fortuna, CG
Přispěvatelé: Musumeci, R, Wiederhold, N, Jorgensen, J, Patterson, T, Bulbarelli, A, Sancini, G, Pace, A, Palumbo Piccionello, A, Fortuna, C, Cocuzza, C
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Popis: Background: MiBIECT is a new oxadiazolyl-oxazolidinone that has been developed by means of chemoinformatic tools, synthesis and biological evaluation. This agent demonstrates potent activity against Gram-positive pathogens, including linezolid-resistant (LZDR) isolates. The aims of this study were to determine the in vitro activity of MiBIECT against a greater number of Gram-positive cocci with various resistant phenotypes, and to evaluate MiBIECT for in vitro cytotoxicity. Methods: A total of 340 strains of linezolid-susceptible (LZD-S) S. aureus, S. epidermidis, enterococci, S. pneumoniae, S. pyogenes and 20 LZDR strains were analyzed. MiBIECT was evaluated for its in vitro antibacterial activity by determining the minimum inhibitory concentrations (MIC) by the CLSI broth microdilution methods. In vitro cytotoxicity assays in cell lines representative of excretory organs were used to evaluate for potential safety concerns. Results: MiBIECT exhibited potent activity against S. aureus, S. epidermidis, S. pneumoniae and S. pyogenes with MICs in range of
Databáze: OpenAIRE